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Description: PI3kdelta inhibitor 1 is a novel, potent and selective PI3Kdelta inhibitor with an IC50 of 3.8 nM. It is >= 200 fold selective for the remaining three Class I PI3K isoforms and additional kinases. It was identified based on the idea that isoform selectivity from the affinity pocket and tryptophan shelf can be obained.The hypothesis for selectivity is illustrated through structure activity relationships and crystal structures of compounds bound to a K802T mutant of PI3Kgamma. Pharmacokinetic data in rats and mice support the use of PI3kdelta inhibitor 1 as a useful tool compound to use for in vivo studies.
References: Bioorg Med Chem Lett. 2012 Jul 1; 22(13):4296-302.
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